U.S. Pat. No. 7,304,036 discloses peptides that act as agonists of the guanylate cyclase C (GC-C) receptor for the treatment of gastrointestinal disorders. One particular peptide disclosed therein is linaclotide, which consists of the following amino acid sequence: Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (SEQ ID NO 1).
U.S. Pat. Nos. 7,304,036 and 7,371,727 disclose methods for the preparation of linaclotide and related peptides. The contents of U.S. Pat. Nos. 7,304,036 and 7,371,727 are incorporated herein by reference, in their entirety.
There remains a need in the art for improved forms of linaclotide having improved properties.
The present invention relates to a new crystalline form or polymorph of linaclotide, which has surprisingly and unexpectedly enhanced properties, such as enhanced or greater stability, as compared to amorphous linaclotide. In addition, such a crystalline form of linaclotide may have enhanced storage stability and enhanced stability against chemical degradation as compared to amorphous linaclotide.